CN111803398B - Acne-removing vesicle composition as well as preparation method and application thereof - Google Patents
Acne-removing vesicle composition as well as preparation method and application thereof Download PDFInfo
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Abstract
The invention discloses an acne-removing vesicle composition as well as a preparation method and application thereof, belonging to the field of cosmetics. The invention combines 7 active ingredients of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, solves the problem of acne from 4 dimensions of adjusting hyperkeratosis of epidermis, controlling oil, sterilization and anti-inflammation, has good treatment effect on common acne from grade I to grade II, and can eliminate acne marks caused by variola inflammation and melanosis; in addition, the 7 active ingredients are embedded in the vesicles, so that the stability of the active ingredients can be improved, and the prepared acne-removing vesicle composition is stable, good in mutual compatibility, good in effect, simple in preparation method and low in cost.
Description
Technical Field
The invention belongs to the field of cosmetics, and relates to an acne removing vesicle composition as well as a preparation method and application thereof.
Background
Acne is a chronic inflammatory skin disease of the sebaceous glands of the hair follicle, and the three common acne are acne vulgaris, acne rosea, and acne vulgaris (commonly referred to as apocrine sweat gland AI/HS) in the United states. Acne vulgaris results from the hyperactivated proliferation of keratinocytes in young healthy follicular units; rosacea weakens the upper parts of the follicular units due to sun damage; AI/HS is caused by the destruction of follicular unit at the interface of pilosebaceous gland, and mainly solves the problem of partial acne vulgaris in the field of daily chemicals.
From the skin microstructure produced by acne, the mechanism of acne production is as follows: the FPSU (pilosebaceous unit) structure is the basic unit for the development of acne and consists of follicular units, hair units and sebaceous units. The FPSU produces a variety of substances-hair, sebum and ductal keratinocytes, of which the hair unit is the smallest associated with acne. The oil secreted by the sebaceous glands is a liquid and does not clog anything. The source of acne is small cells of the vessel wall which slough off in the catheter and then disappear on the surface. When the catheter keratinocytes do not shed, they block the catheter, resulting in acne (acne vulgaris, acne roses, acne vulgaris). While sebum occlusion is a misunderstanding of acne, sebum is a bystander in the inventive process of acne, and sebum is not an innocent bystander, providing food for microorganisms on the skin. That is, when the follicular sebaceous gland intimal epithelial cells are shed not in the form of fine particles but in abnormally large sheets, they are unable to be discharged through the follicular orifice to form a blockage. This process is first detected at the junction of the sebaceous duct and the hair follicle epithelium, and then rapidly spreads to the distal cells. The end result is that the pores are clogged by inclusions of keratin and lipids of the catheter keratinocytes, and then acne occurs.
The initial acne stage of acne is non-inflammatory acne and may remain in the acne stage forever in many patients; inflammatory acne develops when this process extends to the immune system. From the time axis, a pox begins with abnormal keratinization of the follicle, then slowly changes from a micro-powder prick to a blackhead/whitehead, then to a papule/pustule, and then to a nodule/cyst, during which the degree of inflammation gradually increases upwards. Acne is classified by severity as follows:
mild (grade I): acne alone-loose or multiple blackheads, comedones;
medium (grade II): inflammatory papules-except acne, inflammatory papules are evident, multiply confined to the face;
medium (grade III): pustules, which are inflammatory lesions with increased depth in the face, neck and chest;
severe (grade IV): nodules and cysts-nodules and cysts can be accompanied by scar formation.
It follows that acne is produced by hyperkeratosis of the pilosebaceous canal, followed by a series of acne manifestations associated with microbial proliferation, destruction of the pilosebaceous unit, inflammation, etc. When the acne grade is more than or equal to grade III, a doctor generally needs to be seen.
At present, products for treating the acne of the I grade to the II grade generally only have one or two effects of adjusting hyperkeratosis of epidermis, controlling oil, sterilizing and resisting inflammation, so that a product capable of completely removing the acne is needed to be developed.
Disclosure of Invention
In order to solve the disadvantages and shortcomings of the prior art, the present invention provides an anti-acne vesicle composition, a preparation method thereof and an application thereof, which can solve the problem of mild to moderate acne vulgaris from four dimensions of adjusting hyperkeratosis of epidermis, controlling oil, sterilizing and resisting inflammation, and other grades and types of acne are medicinally regarded and are not considered in the scope of the present invention.
In a first aspect, the invention provides an acne removing vesicle composition, which comprises the following components in percentage by weight: 0.1-10% of active matter, 2.3-55% of vesicle component and 35-97.6% of water;
wherein the active substance comprises papain, nicotinamide, zinc gluconate, caprylylglycine, caprylyl glycol, linoleic acid and acetyl chitosamine;
the vesicle components include emulsifier, co-emulsifier, cholesterol and hydrogenated lecithin.
Papain can regulate epidermal hyperkeratosis, nicotinamide, zinc gluconate and acetylchitosamine have the effect of controlling oil, caprylyl glycine and caprylyl glycol have the bactericidal effect, linoleic acid has the anti-inflammatory effect, the active compound can solve the acne problem from 4 dimensions of regulation of epidermal hyperkeratosis, oil control, sterilization and anti-inflammation by combining the 7 raw materials, and has good treatment effect on common acne from grade I to grade II. The active substance has the effect of treating common acne of I grade to II grade, and can eliminate acne marks caused by inflammation of pox and melanosis. In addition, the acne removing vesicle composition embeds the active substance into the vesicle, so that the active substance is more stable.
As a preferred embodiment of the acne vesicle composition of the present invention, the active comprises the following components in parts by weight: 0.5-5 parts of papain, 1-8 parts of nicotinamide, 0.05-5 parts of zinc gluconate, 0.01-5 parts of caprylyl glycine, 0.01-3 parts of caprylyl glycol, 1-10 parts of linoleic acid and 0.1-5 parts of acetyl chitosamine. The 7 active ingredients have better anti-inflammatory effect and acne removing effect than the active ingredients outside the range under the specific proportion.
As a further preferred embodiment of the acne vesicle composition of the invention, the active comprises the following components in parts by weight: 3.8 parts of papain, 5 parts of nicotinamide, 3 parts of zinc gluconate, 3.2 parts of caprylyl glycine, 2.4 parts of caprylyl glycol, 6.5 parts of linoleic acid and 1.8 parts of acetyl chitosamine. Especially, when the 7 active ingredients are in the specific proportion, the anti-inflammatory effect is better, and the acne removing effect is better.
As a preferred embodiment of the acne removing vesicle composition of the invention, the vesicle component comprises the following components in parts by weight: 0.1-10 parts of emulsifier, 2-35 parts of co-emulsifier, 0.1-5 parts of cholesterol and 0.1-5 parts of hydrogenated lecithin. When the vesicle component comprises the components in parts by weight, the active substances can be effectively embedded in the vesicles, and the formed vesicles have very small particle size, very good dispersibility and very good stability.
As a further preferred embodiment of the acne removing vesicle composition of the invention, the vesicle component comprises the following components in parts by weight: 4.5 parts of emulsifier, 15.7 parts of auxiliary emulsifier, 0.24 part of cholesterol and 1.25 parts of hydrogenated lecithin. Under the condition, the obtained vesicles can better embed active ingredients, and the formed vesicles have smaller particle size, better dispersibility and better stability.
As a preferred embodiment of the acne-removing vesicle composition of the invention, the emulsifier comprises polyglycerol-6 laurate and triitant palmitate, wherein the weight ratio of polyglycerol-6 laurate to triitant palmitate is polyglycerol-6 laurate: tricuspid palmitate ═ 1: 0.01-1.2.
As a further preferred embodiment of the acne vesicle composition of the invention, the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is polyglycerol-6 laurate: trinitant palmitate ═ 1: 0.04.
in a second aspect, the invention provides a preparation method of the acne removing vesicle composition, which comprises the following steps:
(1) mixing an emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, and completely dissolving and dispersing under a heating condition to obtain an oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, and uniformly dispersing under heating to obtain water phase;
(3) adding the water phase obtained in the step (2) into the oil phase obtained in the step (1), and stirring for primary emulsification to obtain primary emulsion;
(4) and (4) homogenizing the primary emulsion obtained in the step (3) under high pressure to obtain nano vesicles, so as to obtain the acne-removing vesicle composition.
As a preferred embodiment of the preparation method of the present invention, the heating temperature in the step (1) is 55 to 65 ℃; the heating temperature in the step (2) is 45-55 ℃; the rotating speed of stirring in the step (3) is 6000-12000 r/min; the pressure for high-pressure homogenization in the step (4) is 800-1500bar, and the homogenization frequency is 5-9.
In a third aspect, the invention also provides an application of the acne removing vesicle composition in cosmetics.
Compared with the prior art, the invention has the following advantages: the invention combines 7 active ingredients, namely papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, solves the problem of acne from 4 dimensions of adjusting hyperkeratosis of epidermis, controlling oil, sterilizing and resisting inflammation, has good treatment effect on common acne from grade I to grade II, and can eliminate acne marks caused by variola inflammation and melanosis. In addition, the active ingredients are wrapped in the vesicles, so that the stability of the active ingredients can be improved, and the obtained acne-removing vesicle composition is stable, good in mutual compatibility, good in effect, simple in preparation method and low in cost.
Drawings
FIG. 1 shows the results of the IL-1. beta. inhibition test in Effect example 3.
Detailed Description
To better illustrate the objects, aspects and advantages of the present invention, the present invention is further illustrated by the following examples. It is apparent that the following examples are only a part of the embodiments of the present invention, and not all of them. It should be understood that the embodiments of the present invention are only for illustrating the technical effects of the present invention, and are not intended to limit the scope of the present invention.
Example 1
This example is an embodiment of the acne-removing vesicle composition of the present invention. The acne-removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 21.69 parts of vesicle component and 75.31 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 7 active matters is that the papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 3.8:5:3:3.2:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.24: 1.25;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: trinitant palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition comprises the following steps:
(1) mixing emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, heating to 62 deg.C, and dissolving and dispersing completely to obtain oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, heating to 51 deg.C, and dissolving and dispersing to obtain water phase;
(3) slowly adding the water phase obtained in the step (2) into the oil phase obtained in the step (1) while stirring at 9000r/min to obtain primary emulsion;
(4) and (4) carrying out high-pressure homogenization on the primary emulsion obtained in the step (3) under the conditions that the pressure is 1200bar and the homogenization times are 7 times to obtain nano vesicles, thus obtaining the acne-removing vesicle composition.
Example 2
This example is an embodiment of the acne-removing vesicle composition of the present invention. The acne-removing vesicle composition comprises the following components in parts by weight: 0.1 part of active matter, 3.2 parts of vesicle component and 96.7 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 7 active matters is papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 3.8:5:3:3.2:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 1: 2: 0.1: 0.1;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition comprises the following steps:
(1) mixing emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, heating to 55 deg.C, and dissolving and dispersing completely to obtain oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, heating to 45 deg.C, and dissolving and dispersing to obtain water phase;
(3) slowly adding the water phase obtained in the step (2) into the oil phase obtained in the step (1) while stirring at 6000r/min to obtain primary emulsion;
(4) and (4) carrying out high-pressure homogenization on the colostrum obtained in the step (3) under the conditions of the pressure of 800bar and the homogenization frequency of 9 times to obtain nano vesicles, thus obtaining the acne-removing vesicle composition.
Example 3
This example is an embodiment of the anti-acne vesicle composition of the invention. The acne-removing vesicle composition comprises the following components in parts by weight: 10 parts of active matter, 60 parts of vesicle component and 30 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 7 active matters is papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 3.8:5:3:3.2:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin 15: 35: 5: 5;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition comprises the following steps:
(1) mixing emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, heating to 65 deg.C, and dissolving and dispersing completely to obtain oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, heating to 55 deg.C, and dissolving and dispersing to obtain water phase;
(3) slowly adding the water phase obtained in the step (2) into the oil phase obtained in the step (1) while stirring at 12000r/min to obtain primary emulsion;
(4) and (4) carrying out high-pressure homogenization on the colostrum obtained in the step (3) under the conditions of the pressure of 1500bar and the homogenization frequency of 9 times to obtain nano vesicles, thus obtaining the acne-removing vesicle composition.
Example 4
This example is an embodiment of the acne-removing vesicle composition of the present invention. The acne-removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 20.4 parts of vesicle component and 76.6 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 7 active matters is papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 0.5:1:0.05:0.01:0.01:1: 0.1;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.1: 0.1;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.01.
the preparation method of the acne removing vesicle composition comprises the following steps:
(1) mixing emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, heating to 62 deg.C, and dissolving and dispersing completely to obtain oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, heating to 51 deg.C, and dissolving and dispersing to obtain water phase;
(3) slowly adding the water phase obtained in the step (2) into the oil phase obtained in the step (1) while stirring at 9000r/min to obtain primary emulsion;
(4) and (4) carrying out high-pressure homogenization on the colostrum obtained in the step (3) under the conditions that the pressure is 1200bar and the homogenization frequency is 7 times, so as to obtain nano vesicles, namely the acne-removing vesicle composition.
Example 5
This example is an embodiment of the acne-removing vesicle composition of the present invention. The acne-removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 49.5 parts of vesicle component and 47.5 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 7 active matters is papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 5:8:5:5:3:10: 5;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 35: 5: 5;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 1.2.
the preparation method of the acne-removing vesicle composition comprises the following steps:
(1) mixing emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, heating to 62 deg.C, and dissolving and dispersing completely to obtain oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, heating to 51 deg.C, and dissolving and dispersing to obtain water phase;
(3) slowly adding the water phase obtained in the step (2) into the oil phase obtained in the step (1) while stirring at 9000r/min to obtain primary emulsion;
(4) and (4) carrying out high-pressure homogenization on the colostrum obtained in the step (3) under the conditions that the pressure is 1200bar and the homogenization frequency is 7 times, so as to obtain nano vesicles, namely the acne-removing vesicle composition.
Comparative example 1
The present comparative example provides an anti-acne vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 0.05 part of active matter, 2.6 parts of vesicle component and 97.35 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 7 active matters is papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 3.8:5:3:3.2:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, an auxiliary emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the auxiliary emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 0.5: 2: 0.05: 0.05;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition comprises the following steps:
(1) mixing emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, heating to 50 deg.C, and dissolving and dispersing completely to obtain oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, heating to 40 deg.C, and dissolving and dispersing to obtain water phase;
(3) slowly adding the water phase obtained in the step (2) into the oil phase obtained in the step (1) while stirring at the condition of 5000r/min to obtain primary emulsion;
(4) and (4) carrying out high-pressure homogenization on the colostrum obtained in the step (3) under the conditions that the pressure is 600bar and the homogenization frequency is 5 times to obtain nano vesicles, thus obtaining the acne-removing vesicle composition.
Comparative example 2
The present comparative example provides an acne-removing vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 13 parts of active matter, 70 parts of vesicle component and 17 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 7 active matters is that the papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 3.8:5:3:3.2:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, an auxiliary emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the auxiliary emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 18: 35: 9: 8;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition comprises the following steps:
(1) mixing emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, heating to 70 deg.C, and dissolving and dispersing completely to obtain oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, heating to 70 deg.C, and dissolving and dispersing to obtain water phase;
(3) slowly adding the water phase obtained in the step (2) into the oil phase obtained in the step (1) while stirring at the speed of 15000r/min to obtain primary emulsion;
(4) and (4) carrying out high-pressure homogenization on the colostrum obtained in the step (3) under the conditions of the pressure of 1500bar and the homogenization times of 12 times to obtain nano vesicles, thus obtaining the acne-removing vesicle composition.
Comparative example 3
The present comparative example provides an anti-acne vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 21.69 parts of vesicle component and 75.31 parts of water;
wherein, the active matter consists of nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 6 active matters is nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 5:3:3.2:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.24: 1.25;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.04.
the preparation method of the acne removing vesicle composition in the comparative example has the same steps and process parameters as those in example 1 except that papain is not adopted.
Comparative example 4
The present comparative example provides an acne-removing vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 21.69 parts of vesicle component and 75.31 parts of water;
wherein, the active matter is composed of papain, zinc gluconate, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, the weight ratio of the 6 active matters is that the papain: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 3.8:3:3.2:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.24: 1.25;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: trinitant palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition in the comparative example has the same steps and process parameters as example 1 except that nicotinamide is not adopted.
Comparative example 5
The present comparative example provides an acne-removing vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 21.69 parts of vesicle component and 75.31 parts of water;
wherein, the active matter consists of papain, nicotinamide, caprylyl glycine, caprylyl glycol, linoleic acid and acetyl chitosamine, and the weight ratio of the 6 active matters is that the papain: nicotinamide: capryloyl glycine: and (3) octyl glycol: linoleic acid: chitosamine 3.8:5:3.2:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.24: 1.25;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.04.
the preparation method of the acne removing vesicle composition in the comparative example is the same as that of example 1 except that zinc gluconate is not adopted.
Comparative example 6
The present comparative example provides an anti-acne vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 21.69 parts of vesicle component and 75.31 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycol, linoleic acid and acetyl chitosamine, the weight ratio of the 6 active matters is papain: nicotinamide: zinc gluconate: and (3) octyl glycol: linoleic acid: chitosamine 3.8:5:3:2.4:6.5: 1.8;
the vesicle component consists of an emulsifier, an auxiliary emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the auxiliary emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.24: 1.25;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.04.
the preparation method of the acne removing vesicle composition in the comparative example has the same steps and process parameters as those in example 1 except that caprylyl glycine is not adopted.
Comparative example 7
The present comparative example provides an acne-removing vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 21.69 parts of vesicle component and 75.31 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, linoleic acid and acetyl chitosamine, the weight ratio of the 6 active matters is that the papain: nicotinamide: zinc gluconate: capryloyl glycine: linoleic acid: chitosamine 3.8:5:3:3.2:6.5: 1.8;
the vesicle component consists of an emulsifier, an auxiliary emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the auxiliary emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.24: 1.25;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: trinitant palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition in the comparative example is the same as that of example 1 except that the octyl glycol is not adopted.
Comparative example 8
The present comparative example provides an anti-acne vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 21.69 parts of vesicle component and 75.31 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol and acetyl chitosamine, and the weight ratio of the 6 active matters is papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: chitosamine 3.8:5:3:3.2:2.4: 1.8;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.24: 1.25;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: tricuspid palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition in the comparative example has the same steps and process parameters as those in example 1 except that linoleic acid is not adopted.
Comparative example 9
The present comparative example provides an acne-removing vesicle composition. The acne removing vesicle composition comprises the following components in parts by weight: 3 parts of active matter, 21.69 parts of vesicle component and 75.31 parts of water;
wherein, the active matter consists of papain, nicotinamide, zinc gluconate, caprylyl glycine, caprylyl glycol and linoleic acid, and the weight ratio of the 6 active matters is that the papain: nicotinamide: zinc gluconate: capryloyl glycine: and (3) octyl glycol: linoleic acid 3.8:5:3:3.2:2.4: 6.5;
the vesicle component consists of an emulsifier, a co-emulsifier, cholesterol and hydrogenated lecithin, and the weight ratio of the emulsifier to the co-emulsifier is as follows: auxiliary emulsifier: cholesterol: hydrogenated lecithin ═ 4.5: 15.7: 0.24: 1.25;
the emulsifier consists of polyglycerol-6 laurate and triquetrum palmitate, and the weight ratio of the polyglycerol-6 laurate to the triquetrum palmitate is as follows: trinitant palmitate ═ 1: 0.04.
the preparation method of the acne-removing vesicle composition of the comparative example is the same as that of example 1 except that the acetyl chitosamine is not adopted.
Effect example 1: embedding Performance test
Respectively weighing a certain amount of the acne-removing vesicle compositions prepared in the embodiments 1-5 and the comparative examples 1-9, dissolving a proper amount of distilled water in water, placing the mixture in a centrifuge tube after full dissolution, centrifuging the mixture for 60 minutes at 3000r/min, taking out supernatant liquid by using an injector, adding a proper amount of ethanol or methanol to perform constant volume, measuring the amount of unencapsulated free nicotinamide by using a high performance liquid chromatography (except that the zinc gluconate content in the comparative example 2 is measured, all other components are added with nicotinamide, so that the encapsulation rate of the whole active substance is replaced by the encapsulation rate of nicotinamide), and measuring the particle size, the polydispersity index (PDI) and the Zeta potential by using Malven Zetasizer Nano ZS90 at room temperature. The results are shown in Table 1.
TABLE 1
| Sample(s) | Embedding rate | Particle size nm | Polydispersity index PDI | Zeta potential mV |
| Example 1 | 95.46％ | 110.1 | 0.107 | -17.1 |
| Example 2 | 90.14％ | 113.7 | 0.115 | -16.0 |
| Example 3 | 70.52％ | 130.14 | 0.1965 | -12.0 |
| Example 4 | 76.46％ | 117.4 | 0.161 | -13.1 |
| Example 5 | 78.14％ | 127.1 | 0.144 | -14.5 |
| Comparative example 1 | 64.78％ | 200.1 | 0.214 | -9.4 |
| Comparative example 2 | 43.13％ | 328.5 | 0.324 | -4.8 |
| Comparative example 3 | 56.21％ | 277.3 | 0.257 | -6.7 |
| Comparative example 4 | 58.62％ | 276.2 | 0.271 | -6.1 |
| Comparative example 5 | 48.13％ | 261.1 | 0.304 | -5.3 |
| Comparative example 6 | 53.21％ | 289.9 | 0.298 | -5.9 |
| Comparative example 7 | 54.31％ | 280.9 | 0.299 | -5.8 |
| Comparative example 8 | 56.22％ | 281.1 | 0.297 | -6.0 |
| Comparative example 9 | 56.13％ | 283.1 | 0.290 | -5.5 |
The results in table 1 show that the nanovesicle compositions prepared in the examples of the present invention have higher encapsulation efficiency compared to the comparative examples, and the nanovesicle compositions of the examples have better dispersibility and higher potential resistance. Wherein the embedding rate of the sample is 95.46% and the particle size is only 110.1nm as measured in example 1.
Effect example 2: stability test
Taking the acne removing vesicle compositions prepared in examples 1-5 and comparative examples 1-9, respectively measuring the particle size and the nicotinamide or zinc gluconate content of each sample (the zinc gluconate content is measured in comparative example 2, and the nicotinamide content is measured in all the other samples); then, storing each sample at 4 ℃ and 50 ℃, sampling after 1 month, re-measuring the particle size and the content of the nicotinamide or zinc gluconate (measuring the content of the zinc gluconate in comparative example 2, and measuring the content of the nicotinamide in all other samples), and calculating the content change of the nicotinamide in each sample; in addition, each sample is respectively taken to be centrifuged for 30min at the rotating speed of 10000r/min, and whether the sample is layered or precipitated is observed; the results of testing each sample are shown in table 2 below.
TABLE 2
As can be seen from table 2, the anti-acne vesicle compositions prepared in the examples have good stability after being stored for 1 month at different temperatures, and the content change and particle size change effects are obviously superior to those of comparative examples 1 to 9, wherein the content and particle size of the composition in example 1 are not significantly changed after being stored for one month at 4 ℃ and 50 ℃, and no delamination or precipitation is observed after centrifugation.
Effect example 3: anti-inflammatory Performance test
The propionibacterium acnes is used for stimulating the THP-1 of the acute mononuclear cells of the human, a specific acne inflammatory cell model is established for detecting the secretion of interleukin 1 beta (IL-1 beta) of an inflammatory factor human, and therefore the anti-inflammatory and anti-acne functions of the acne-removing vesicle composition in the embodiment/the comparative example are evaluated.
The MTT method is used for detecting the influence of the test substance on the survival rate of HDF-a cells, and the subsequent efficacy screening experiment is carried out according to the maximum safe mass concentration of the test substance.
Taking 1 × 10 cells in exponential growth phase 5 one/mL, inoculated in 96-well culture plates at 100. mu.L/well in CO at 37 ℃ 2 Culturing in an incubator. Taking supernatant after 24h, and centrifuging for 10min at 3000 r/min. After centrifugation, taking the supernatant for experiment according to the kit specification, and reacting with a biotin-labeled antibody, HRP-labeled streptavidin, a chromogenic substrate and stop solution in sequence. The blank wells were zeroed and the OD measured at 450nm wavelength for each well within 15min after termination. And calculating a regression equation of the standard curve according to the concentration of the standard substance and the corresponding OD value, and calculating the corresponding concentration Col-I according to the OD value of the sample, wherein the final concentration is the product of the actual measured concentration and the dilution multiple.
Taking cells in exponential growth phase, regulating cell density to about 1 × 10 with culture solution 6 And (8) m L, inoculating the mixture into a 96-well culture plate, and incubating the mixture with the maximum safe concentration of the test object for 4 hours. Taking propionibacterium acnes cultured for 72 hours in an anaerobic way, centrifuging at 2500r/min, washing for 3-4 times by using a PBS solution to prepare a viable bacteria suspension, adding the propionibacterium acnes and THP-1 cells according to the proportion of 100: 1 of the number of the cells, taking incubation without drugs as a negative control, adding retinoic acid (20 mu mol/L) for incubation as a positive control, and only adding Phosphate Buffer Solution (PBS) for blank control. Placing at 37 deg.C with 5% CO 2 And culturing in an incubator with saturated humidity for 24 h. The IL-1 beta content was detected according to the IL-1 beta ELISA kit instructions.
The IL-1 β inhibitory rate is expressed as a secretion amount decrease value/initial secretion amount value × 100%.
The specific results are shown in FIG. 1. The secretion of inflammatory factors is a visual indicator of the occurrence of acne inflammation. Since human acute monocytic THP-1 produces IL-1 beta specifically in response to inflammation, IL-1 beta is generally used as an index for acne inflammation-related screening. As can be seen from fig. 1, the inhibition ratio of the acne removing vesicle composition of example 1 to IL-1 β is substantially consistent with that of the positive control, and the acne removing vesicle composition of each example has a good anti-inflammatory effect, and the inhibition ratio to IL-1 β is obviously better than that of each proportion.
Finally, it should be noted that the above embodiments are only used for illustrating the technical solutions of the present invention and not for limiting the protection scope of the present invention, and although the present invention is described in detail with reference to the preferred embodiments, it should be understood by those skilled in the art that modifications or equivalent substitutions can be made on the technical solutions of the present invention without departing from the spirit and scope of the technical solutions of the present invention.
Claims (5)
1. The acne-removing vesicle composition is characterized by comprising the following components in percentage by weight: 0.1-3% of active matter, 3.2-21.69% of vesicle component and 75.31-96.7% of water; the active matter comprises the following components in parts by weight: 3.8 parts of papain, 5 parts of nicotinamide, 3 parts of zinc gluconate, 3.2 parts of caprylyl glycine, 2.4 parts of caprylyl glycol, 6.5 parts of linoleic acid and 1.8 parts of acetyl chitosamine; the vesicle component comprises the following components in parts by weight: 0.1-15 parts of emulsifier, 2-35 parts of co-emulsifier, 0.1-5 parts of cholesterol and 0.1-5 parts of hydrogenated lecithin; the emulsifier comprises polyglycerol-6 laurate and triquetiapine palmitate, wherein the weight ratio of the polyglycerol-6 laurate to the triquetiapine palmitate is polyglycerol-6 laurate: triquetrum palmitate = 1: 0.01-1.2; the preparation method of the acne removing vesicle composition comprises the following steps:
(1) mixing an emulsifier, cholesterol, hydrogenated lecithin, caprylyl glycine and linoleic acid, and completely dissolving and dispersing under a heating condition to obtain an oil phase;
(2) mixing co-emulsifier, papain, nicotinamide, zinc gluconate, caprylyl glycol, acetyl chitosan and water, and dispersing under heating to obtain water phase;
(3) adding the water phase obtained in the step (2) into the oil phase obtained in the step (1), and stirring for primary emulsification to obtain primary emulsion;
(4) and (4) homogenizing the primary emulsion obtained in the step (3) under high pressure to obtain nano vesicles, so as to obtain the acne-removing vesicle composition.
2. The anti-acne vesicle composition according to claim 1, wherein the vesicle component comprises the following components in parts by weight: 4.5 parts of emulsifier, 15.7 parts of auxiliary emulsifier, 0.24 part of cholesterol and 1.25 parts of hydrogenated lecithin.
3. The anti-acne vesicle composition according to claim 1, wherein the weight ratio of polyglycerol-6 laurate to triquetiapine palmitate is polyglycerol-6 laurate: triquetrum palmitate = 1: 0.04.
4. the acne-removing vesicle composition according to claim 1, wherein the heating temperature in step (1) is 55-65 ℃; the heating temperature in the step (2) is 45-55 ℃; the rotating speed of stirring in the step (3) is 6000-12000 r/min; the pressure of high-pressure homogenization in the step (4) is 800-1500bar, and the homogenization time is 5-9.
5. Use of an anti-acne vesicle composition according to any of claims 1 to 4 in cosmetics.
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| CN108473484A (en) * | 2015-10-01 | 2018-08-31 | 赛诺米克斯公司 | It can be used as the compound of TRPM8 conditioning agents |
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| CN107998978B (en) * | 2017-12-11 | 2019-08-06 | 江南大学 | A kind of composition, preparation and the application of magnetic liposome vesica |
| CN109316438A (en) * | 2018-08-30 | 2019-02-12 | 珀莱雅化妆品股份有限公司 | A kind of preparation method of the solid precursor liposome with acne-removing |
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| CN108473484A (en) * | 2015-10-01 | 2018-08-31 | 赛诺米克斯公司 | It can be used as the compound of TRPM8 conditioning agents |
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